三尖杉茎叶中黄酮类化合物的研究

目的 研究三尖杉(Cephalotaxus fortunei Hook.f.)茎叶的化学成分。方法 运用硅胶、ODS、Sephadex LH-20凝胶柱色谱以及高效液相制备色谱等分离技术，对三尖杉茎叶75%(体积分数)乙醇提取物的二氯甲烷、乙酸乙酯和正丁醇萃取部位的化学成分进行分离，并根据化合物理化性质及波谱数据进行结构鉴定。结果 从三尖杉茎叶75%(体积分数)乙醇提取物中分离得到15个黄酮类化合物，分别鉴定为芹菜素(1)、木犀草素(2)、山柰酚(3)、槲皮素(4)、大豆素(5)、柚皮素(6)、圣草酚(7)、二氢山柰酚(8)、6-methylaromadendrin(9)、芹菜素苷(10)、芹菜素-6-C-甲基-7-O-β-D-吡喃葡萄糖苷(11)、柯伊利素-7-O-β-D-吡喃葡萄糖苷(12)、香叶木素-7-O-β-D-吡喃葡萄糖苷(13)、去甲杜鹃素(14)和2,3-二氢-6-甲基银杏素(15)。结论 化合物2、7、9、12和13为首次从三尖杉属植物中分离得到，化合物3～6、8、10、11、14和15为首次从三尖杉中分离得到。     

金银忍冬叶的化学成分研究

目的 研究金银忍冬叶Lonicera macckii (Rupr.) Maxim.的化学成分.方法 采用硅胶柱色谱、Sephadex LH-2柱色谱、重结晶等方法进行分离纯化,根据理化性质和波谱数据鉴定化合物的结构.结果 从金银忍冬叶中分离鉴定了12个化合物,分别为山柰酚(1)、芹菜素(2)、金丝桃苷(3)、芹菜素-7-O-β-D-吡喃葡萄糖苷(4)、金圣草素-4′-O-β-D-葡萄糖苷(5)、木犀草素-7-O-β-D-吡喃葡萄糖苷(6)、裂环马钱素酸(7)、獐牙菜苷(8)、3,5-O-二咖啡酰基奎宁酸甲酯(9)、齐墩果酸(10),胡萝卜苷(11)、β-谷甾醇(12).结论 化合物1～6、8～12为首次从该植物中分离得到,化合物5为首次从该属植物中分离得到.     

海南核果木中苯丙素类化学成分的分离与鉴定

目的研究海南核果木(Drypetes hainanensis Merr.)枝叶中苯丙素类化学成分。方法通过多种色谱技术进行分离纯化,包括硅胶柱色谱、Sephadex LH-20柱色谱、MCI、高效液相色谱等方法,利用理化数据和波谱技术分析确定化合物的结构。结果与结论从海南核果木干燥枝叶的正丁醇提取物中分离得到8个已知苯丙素类化合物,分别鉴定为erythro-7-methoxyguaiacylglycerol(1)、threo-7-methoxyguaiacylglycerol(2)、erythro-7-methoxysyringylglycerol(3)、threo-7-methoxysyringylglycerol(4)、erythro-guaiacylglycerol(5)、threo-guaiacylglycerol(6)、erythro-syringylglycerol(7)、threo-syringylglycerol(8)。所有化合物均为首次从该植物中分离得到。     

蔓性千斤拔的化学成分研究

目的研究蔓性千斤拔(Moghania philippinensis)根的95%(体积分数)乙醇提取物的化学成分。方法采用制备薄层色谱、反复硅胶柱色谱、Sephadex LH-20柱色谱、开放ODS柱色谱等方法进行分离纯化;根据理化性质及波谱分析鉴定化合物的结构。结果与结论从蔓性千斤拔中分离得到9个已知化合物,分别鉴定为大豆素(1)、染料木素(2)、3'-O-methylorobol(3)、2'-羟基染料木素(4)、aureol(5)、lupinalbin A(6)、山柰酚(7)、questin(8)、羽扇豆醇(9)。化合物7、8为首次从该属植物中分离得到,化合物5为首次从该植物中分离得到。     

中华卷柏木脂素类化学成分研究

目的研究中华卷柏中木脂素类化合物。方法采用硅胶、聚酰胺、LH-20柱色谱和半制备高效液相等现代色谱分离技术对中华卷柏75%乙醇提取液进行分离纯化,根据化合物的理化性质和波谱数据进行结构鉴定。结果从中华卷柏75%乙醇提取液中分离并鉴定了4个木脂素类化合物,分别为(7R,8S)-ceplignan(1)、2,3-trans-3,4-trans-2-methoxy-3-hydroxymethyl-4-[bis-(4-hydroxyphenyl)methyl]tetrahydrofuran(2)、(8S,8'R,7'R)-[tetrahydro-5-(3-hydroxy-4-methoxyphenyl)-4-(hydroxymethyl)-3-furanyl]-3-hydroxy-4-methoxyphenyl-methanone(3)、(+)-isolariciresinol(4)。结论化合物1、3、4是首次从该植物中分离得到,化合物3是首次在卷柏属植物中被发现。     

苦瓜茎叶醋酸乙酯部位的化学成分研究

目的研究苦瓜茎叶醋酸乙酯部位的化学成分,为进一步开发利用苦瓜茎叶提供依据。方法采用反复硅胶柱色谱、反相ODS柱色谱、Sephadex LH-20等柱色谱进行分离纯化,并根据波谱数据鉴定化合物的结构。结果分离得到3种苦瓜三萜,分别鉴定为苦瓜素I(1)、kuguacin N(2)、3,7-二羟基-23(R)-乙氧基-19-醛基-5,24-二烯醇(3)。结论化合物3为新化合物,命名为23-乙基苦瓜素I。     

南天竹种子中木脂素类成分研究

目的研究南天竹种子的化学成分。方法采用正相硅胶、凝胶、微孔树脂、半制备高效液相柱色谱等手段分离,波谱法进行结构鉴定。结果从南天竹种子中分离得到7个木脂类化合物:丁香脂素(1)、松脂素(2)、杜仲树脂酚(3)、1-羟基松脂素(4)、gentioluteol(5)、berchemol(6)、berchemol-4’-O-β-D-吡喃葡萄糖苷(7)。结论化合物1~7均为首次从该植物中分离得到。     

锦灯笼中酸浆苦素类化学成分的研究

目的 研究锦灯笼95％乙醇提取物的石油醚、氯仿、醋酸乙酯萃取部位中化学成分.方法 利用硅胶柱色谱、反相ODS柱色谱、制备液相色谱等方法进行分离、纯化,根据化合物的理化性质和光谱数据鉴定其结构.结果 分离得到了7个化合物,经结构鉴定分别为酸浆苦素A(1)、酸浆苦素D(2)、酸浆苦素L(3)、酸浆苦素O(4)、木犀草素(5...     

芫花醋酸乙酯部位的化学成分研究

目的 研究芫花中醋酸乙酯部位化学成分.方法 分别采用聚酰胺柱色谱、硅胶柱色谱、Sephadex LH-20柱色谱等分离技术对芫花醋酸乙酯部位进行分离纯化,根据波谱数据和理化性质确定化合物的结构.结果 从芫花醋酸乙酯部位分离得到11个化合物,分别鉴定为松脂醇(1)、(一)-异落叶松脂素(2)、落叶松脂醇(3)、对羟基苯甲酸(4)、3,4-二羟基苯甲酸(5)、山柰酚-3-β-D-(6-O-反-p-香豆酰)葡萄糖苷(6)、山柰酚-3-β-D-(6-O-顺-p-香豆酰)葡萄糖苷(7)、芫花素(8)、3′-羟基芫花素(9)、芹菜素(10)、木犀草素(11).结论 化合物2、5、7为首次从该植物中分离得到.     

多序岩黄芪化学成分研究

目的研究多序岩黄芪的化学成分.方法用柱色谱分离,用理化性质及波谱方法鉴定结构.结果从多序岩黄芪中分离鉴定了5个化合物:红芪木脂素A(1),异甘草素(2),7-羟基-4′-甲氧基异黄酮(3),毛蕊异黄酮(4)和芒柄花素(5).结论化合物1为新化合物,命名为红芪木脂素A.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.